CA3102214A1 - Ligands to cereblon (crbn) - Google Patents

Ligands to cereblon (crbn) Download PDF

Info

Publication number
CA3102214A1
CA3102214A1 CA3102214A CA3102214A CA3102214A1 CA 3102214 A1 CA3102214 A1 CA 3102214A1 CA 3102214 A CA3102214 A CA 3102214A CA 3102214 A CA3102214 A CA 3102214A CA 3102214 A1 CA3102214 A1 CA 3102214A1
Authority
CA
Canada
Prior art keywords
compound
optionally substituted
formula
mmol
pharmaceutically acceptable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3102214A
Other languages
English (en)
French (fr)
Inventor
Nathanael Gray
Tinghu Zhang
Eric Fischer
Zhixiang HE
Guangyan DU
Katherine DONOVAN
Radoslaw Nowak
Jing Ting Christine YUAN
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Dana Farber Cancer Institute Inc
Original Assignee
Dana Farber Cancer Institute Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Dana Farber Cancer Institute Inc filed Critical Dana Farber Cancer Institute Inc
Publication of CA3102214A1 publication Critical patent/CA3102214A1/en
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Immunology (AREA)
CA3102214A 2018-06-29 2019-06-27 Ligands to cereblon (crbn) Pending CA3102214A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862692167P 2018-06-29 2018-06-29
US62/692,167 2018-06-29
PCT/US2019/039555 WO2020006264A1 (en) 2018-06-29 2019-06-27 Ligands to cereblon (crbn)

Publications (1)

Publication Number Publication Date
CA3102214A1 true CA3102214A1 (en) 2020-01-02

Family

ID=68987146

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3102214A Pending CA3102214A1 (en) 2018-06-29 2019-06-27 Ligands to cereblon (crbn)

Country Status (8)

Country Link
US (2) US11530219B2 (enExample)
EP (1) EP3813829A4 (enExample)
JP (2) JP7321194B2 (enExample)
KR (2) KR20210025061A (enExample)
CN (1) CN112638380B (enExample)
AU (1) AU2019294835B2 (enExample)
CA (1) CA3102214A1 (enExample)
WO (1) WO2020006264A1 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2894994C (en) 2012-12-21 2019-11-12 National Institute Of Radiological Sciences Compounds for imaging tau proteins that accumulate in brain
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
KR20210018199A (ko) 2018-03-26 2021-02-17 씨4 테라퓨틱스, 인코포레이티드 이카로스의 분해를 위한 세레블론 결합제
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
JP7293343B2 (ja) 2018-05-09 2023-06-19 アプリノイア セラピューティクス リミテッド ヘテロアリール化合物及びその使用
CN112638380B (zh) * 2018-06-29 2024-05-24 达纳-法伯癌症研究所有限公司 小脑蛋白(crbn)配体
KR20220100921A (ko) 2019-11-13 2022-07-18 아프리노이아 테라퓨틱스 리미티드 타우 단백질 응집체를 분해하기 위한 화합물 및 이의 용도
EP4076464A4 (en) * 2019-12-17 2024-06-12 Orionis Biosciences, Inc. COMPOUNDS FOR MODULATION OF PROTEIN RECRUITMENT AND/OR DEGRADATION
IL293530A (en) 2019-12-18 2022-08-01 Novartis Ag Derivatives of 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione and their uses
US20230203022A1 (en) * 2020-04-30 2023-06-29 Shanghaitech University Heterocycle and glutarimide skeleton-based compound and applications thereof
WO2022152821A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
AR126052A1 (es) 2021-06-03 2023-09-06 Novartis Ag Derivados de 3-(5-oxi)-1-oxoisoindolin-2-il)piperidina-2,6-diona y sus usos
CN115504963A (zh) * 2021-06-22 2022-12-23 苏州开拓药业股份有限公司 一种c-Myc蛋白降解剂
WO2022272061A1 (en) * 2021-06-25 2022-12-29 Celgene Corporation Cereblon binding compounds, compositions thereof, and methods of treatment therewith
WO2023081400A1 (en) * 2021-11-04 2023-05-11 The Brigham And Women’S Hospital, Inc. Directed degron molecules and applications thereof
EP4452414A2 (en) * 2021-12-22 2024-10-30 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
CA3237577A1 (en) 2021-12-22 2023-06-29 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
KR102738668B1 (ko) 2022-02-25 2024-12-06 계명대학교 산학협력단 항암 활성을 갖는 신규 화합물 및 이의 용도
WO2023178181A1 (en) 2022-03-17 2023-09-21 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
IL316803A (en) 2022-06-06 2025-01-01 C4 Therapeutics Inc Bicyclic glutarimide-modified cervalon-binding agents
JP2025537152A (ja) 2022-11-04 2025-11-14 ブリストル-マイヤーズ スクイブ カンパニー 異常ヘモグロビン症の治療のための化合物およびその使用
WO2024167423A1 (en) * 2023-02-07 2024-08-15 Captor Therapeutics S.A. Gspt1 degrader compounds
TW202500195A (zh) * 2023-05-18 2025-01-01 美商飛爾富來生物公司 異吲哚啉酮-戊二醯亞胺抗體結合物及其用途
WO2025101912A1 (en) * 2023-11-09 2025-05-15 The Board Of Trustees Of The Leland Stanford Junior University Hells helicase degraders and uses thereof

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
KR20060109979A (ko) * 2003-12-02 2006-10-23 셀진 코포레이션 혈색소병증 및 빈혈의 치료 및 관리를 위한 방법및 조성물
KR101164696B1 (ko) * 2004-04-14 2012-07-11 셀진 코포레이션 골수이형성 증후군의 치료 및 관리를 위한 면역조절화합물의 사용 방법 및 상기 화합물을 포함하는 조성물
BRPI0614995A2 (pt) 2005-08-31 2010-01-12 Celgene Corp composto ou um sal, solvato ou estereoisemero farmaceuticamente aceitável do mesmo, composição farmacêutica, uso de uma quantidade terapêutica ou profilaticamente eficaz de um composto ou um sal, solvato ou estereoisemero farmaceuticamente aceitável do mesmo, e, forma de dosagem unitária única
BRPI0720264B1 (pt) 2006-12-08 2022-03-03 Novartis Ag Compostos e composições como inibidores de proteína cinase
PE20140963A1 (es) 2008-10-29 2014-08-06 Celgene Corp Compuestos de isoindolina para el tratamiento de cancer
CN101580501B (zh) 2009-06-01 2011-03-09 南京卡文迪许生物工程技术有限公司 3-(取代二氢异吲哚酮-2-基)-2,6-哌啶二酮的合成方法及其中间体
KR20250127179A (ko) * 2014-04-14 2025-08-26 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
JP6640126B2 (ja) 2014-06-27 2020-02-05 セルジーン コーポレイション セレブロン及び他のe3ユビキチンリガーゼの立体構造の変化を誘導するための組成物及び方法
US9499514B2 (en) * 2014-07-11 2016-11-22 Celgene Corporation Antiproliferative compounds and methods of use thereof
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
AU2019284608A1 (en) 2018-06-13 2020-12-17 Biotheryx, Inc. Aminoamide compounds
CN112638380B (zh) 2018-06-29 2024-05-24 达纳-法伯癌症研究所有限公司 小脑蛋白(crbn)配体

Also Published As

Publication number Publication date
US20230312575A1 (en) 2023-10-05
JP7321194B2 (ja) 2023-08-04
CN112638380A (zh) 2021-04-09
AU2019294835A1 (en) 2020-12-17
EP3813829A1 (en) 2021-05-05
JP2023139195A (ja) 2023-10-03
WO2020006264A1 (en) 2020-01-02
US12110292B2 (en) 2024-10-08
CN112638380B (zh) 2024-05-24
EP3813829A4 (en) 2021-12-08
KR20250020690A (ko) 2025-02-11
KR20210025061A (ko) 2021-03-08
JP2021530451A (ja) 2021-11-11
JP7631434B2 (ja) 2025-02-18
AU2019294835B2 (en) 2025-04-17
US11530219B2 (en) 2022-12-20
US20210292325A1 (en) 2021-09-23

Similar Documents

Publication Publication Date Title
US12110292B2 (en) Ligands to cereblon (CRBN)
AU2019220632B2 (en) IRAK degraders and uses thereof
AU2019293235B2 (en) Immunomodulatory compounds
AU2019294836B2 (en) Bispecific degraders
EP3813834A1 (en) New crbn modulators
CA3150316A1 (en) ERK5 DEGRADING AGENTS USED AS THERAPEUTIC AGENTS IN CANCER AND INFLAMMATORY DISEASES
US20240376096A1 (en) Small molecule cyclin dependent kinase 4/6 (cdk4/6) and ikzf2 (helios) degraders and methods of use thereof
CA3132348A1 (en) Degraders of fibroblast growth factor receptor 2 (fgfr2)
AU2019346595B2 (en) Macrocyclic inhibitors of ALK, TRKA, TRKB, TRKC and ROS1
US20230226196A1 (en) Compounds for targeted degradation of interleukin-2-inducible t-cell kinase and methods of use